Assay Detail
Binding
CHEMBL3366540
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transactivation of human full-length PXR transfected in human HepG2 cells after 24 hrs by luciferase reporter gene assay
17
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Nuclear receptor subfamily 1 group I member 2 (CHEMBL3401) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 5.06 | 5.64 |
| EC20 | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2398716 | — | — | 1 | 5.64 |
| CHEMBL3334727 | — | — | 1 | 5.24 |
| CHEMBL3334822 | — | — | 1 | 5.11 |
| CHEMBL3334815 | — | — | 1 | 4.72 |
| CHEMBL3334825 | — | — | 1 | 4.60 |
| CHEMBL3334725 | — | — | 1 | - |
| CHEMBL3334726 | — | — | 1 | - |
| CHEMBL3334728 | — | — | 1 | - |
| CHEMBL3334816 | — | — | 1 | - |
| CHEMBL3334817 | — | — | 1 | - |
| CHEMBL3334724 | — | — | 1 | - |
| CHEMBL3334819 | — | — | 1 | - |
| CHEMBL3334820 | — | — | 1 | - |
| CHEMBL3334821 | — | — | 1 | - |
| CHEMBL3334823 | — | — | 1 | - |
| CHEMBL3334824 | BMS-817399 | 2.0 | 1 | - |
| CHEMBL3334818 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2398716 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3334727 | — | EC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL3334822 | — | EC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL3334815 | — | EC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL3334825 | — | EC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL3334725 | — | EC20 | = | 7.1 | uM | - |
| CHEMBL3334726 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL3334728 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL3334816 | — | EC20 | = | 5.2 | uM | - |
| CHEMBL3334817 | — | EC20 | = | 8.7 | uM | - |
| CHEMBL3334724 | — | EC50 | - | — | - | |
| CHEMBL3334819 | — | EC20 | = | 0.8 | uM | - |
| CHEMBL3334820 | — | EC50 | - | — | - | |
| CHEMBL3334821 | — | EC50 | > | 25000.0 | nM | - |
| CHEMBL3334823 | — | EC50 | > | 25000.0 | nM | - |
| CHEMBL3334824 | BMS-817399 | EC50 | > | 25000.0 | nM | - |
| CHEMBL3334818 | — | EC20 | = | 2.2 | uM | - |